BMS-986260

BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM) . BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively[1].

Product Specifications

CAS Number

[2001559-19-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

TGF-β Receptor

Type

Reference compound

Related Pathways

TGF-beta/Smad

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/bms-986260.html

Purity

99.95

Solubility

DMSO : ≥ 100 mg/mL

Smiles

N#CC1=CN=C2C=CC(C3=C(C4=CC=C(F)C(Cl)=C4)N=CN3CCO)=NN21

Molecular Formula

C18H12ClFN6O

Molecular Weight

382.78

Precautions

H302, H315, H319, H335

References & Citations

[1]Velaparthi U, et al. Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent. ACS Med Chem Lett. 2020;11 (2) :172-178. Published 2020 Jan 28.